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1: Bioorg Med Chem Lett. 2004 Aug 16;14(16):4197-201.Click here to read Links

Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.

Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.navarre@aventis.com

A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for P4 ligands in combination with a neutral biaryl P1 ligand were investigated with the 2-carboxyindole scaffold. A diverse set of P4 substituents was identified, which, in conjunction with a biaryl P1 ligand, gave highly potent factor Xa inhibitors, which were also selective versus other proteases and efficacious in various antithrombotic secondary assays.

PMID: 15261269 [PubMed - indexed for MEDLINE]